Referenced in: none

Automatically associated channels: Kv10.1

Title: Histidine modification with diethylpyrocarbonate induces a decrease in the binding of an antagonist, PK 11195, but not of an agonist, RO5-4864, of the peripheral benzodiazepine receptors.

Authors: J Benavides, F Bégassat, T Phan, C Tur, A Uzan, C Renault, M C Dubroeucq, C Gueremy, G Le Fur

Journal, date & volume: Life Sci., 1984 Sep 17 , 35, 1249-56

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/6090832

Abstract
[3H]PK 11195 binding to peripheral type benzodiazepine binding sites in kidney membranes is inhibited by the histidine blocking agent diethylpyrocarbonate. This reagent irreversibly decreases the Bmax for [3H]PK 11195 without affecting the affinity. By contrast binding of [3H]RO5-4864 is not affected by diethylpyrocarbonate treatment. However RO5-4864 can protect in a concentration dependent manner the [3H]PK 11195 binding site from diethylpyrocarbonate whereas clonazepam and RO15-1788 are not active. These results suggest that PK 11195 and RO5-4864 interact with different conformational states of the receptors that RO5-4864. This is in agreement with our previous hypothesis that PK 11195 is an antagonist and RO5-4864 an agonist at the "peripheral type" benzodiazepine receptors.